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Fidaxomicin solid dispersion and preparation method thereof

A technology of solid dispersion and fidaxomicin, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. It can solve the problems of not giving the optimal preparation prescription and achieve increased dissolution The effects of high stability, increased concentration, and simple preparation process

Inactive Publication Date: 2015-04-29
BRIGHTGENE BIO MEDICAL TECH (SUZHOU) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent CN101128114B only discloses that the composition containing fidaxomicin can be a tablet, capsule or suspension, but does not give a preferred formulation prescription

Method used

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  • Fidaxomicin solid dispersion and preparation method thereof
  • Fidaxomicin solid dispersion and preparation method thereof
  • Fidaxomicin solid dispersion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1 Preparation of Solid Dispersion Comprising Fidaxomycin and HPMCP

[0047] Dissolve 10g of fidaxomicin in 10ml of ethanol, stir well; slowly add 25ml of ethanol solution into the container, then slowly add 50g of HPMCP (HP55) into the above ethanol solution, stir to obtain a balanced solution, and then add Slowly add 25ml of dichloromethane into the ethanol solution of HPMC, stir and mix evenly, and spray dry with a spray dryer (B-191 miniature spray dryer, Buchi Co., Switzerland). The temperature is 75°C, after drying, cooling, and collecting the powder to obtain a solid dispersion of Fidaxomycin.

Embodiment 2

[0048] Example 2 The Fidaxomycin solid dispersion prepared in Example 1 is mixed in proportion with the following adjuvants to prepare tablets

[0049] The fidaxomicin solid dispersion prepared in Example 1 and colloidal silicon dioxide were sieved through a 30-mesh sieve and fully mixed. Then, 50% sodium carmellose and other components except magnesium stearate and talc in the following table 1 were added thereto, mixed, dried and granulated, and obtained uniformly sized granules by a 25-mesh sieve. Subsequently, the remaining 50% of sodium carboxymethylcellulose, magnesium stearate and talc were added thereto and thoroughly mixed uniformly, the mixture was made into tablets, and the content of each fidaxomicin was 200 mg.

[0050] Table 1:

[0051]

Embodiment 3

[0052] Example 3 Preparation of Solid Dispersion Comprising Fidaxomycin and HPMCAS

[0053] Co-rotating twin-screw extruder TE-20 (Coperon Keya, Germany) was used to set the temperature from each section to the head. After 20 minutes of equilibrium, the screw speed was set to 25r / min, and fidaxomicin and Put 200g of the physical mixture of HPMCAS 1:10 (mass ratio) into the hopper, and after 1min, the die hole of the material head is extruded in strips, and the extrudate is placed on a glass plate, cooled to room temperature and placed for 4 hours , crushed, and passed through a 80-mesh sieve to obtain a white powder.

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PUM

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Abstract

The invention relates to the field of pharmaceutic preparations, in particular to a solid dispersion of fidaxomicin serving as a treating medicament for a disease caused by clostridium difficile and a preparation method for the solid dispersion. The fidaxomicin solid dispersion is solid powder obtained by highly dispersing fidaxomicin into enteric-soluble or water-soluble carrier material, so that the solubility of the fidaxomicin at the small intestine part is greatly improved; compared with a commercially available oral tablet, the fidaxomicin solid dispersion has the advantages of good antibacterial effect, long acting time and little side effect. A medicine composition containing the fidaxomicin solid dispersion provided by the invention is high in solubility and high in stability; the preparation process is simple, the quality is stable, and the fidaxomicin solid dispersion is suitable for industrial production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a fidaxomicin solid dispersion and a preparation method thereof. Background technique [0002] Clostridium difficile diarrhea (CDAD) is a disease characterized by severe and painful diarrhea. Currently, there are two main therapies for CDAD: vancomycin and metronidazole. Vancomycin is not recommended as a first-line drug for the treatment of CDAD because it has antibacterial activity only against some serious life-threatening multidrug-resistant bacteria. Health organizations advise against using this medicine unless absolutely necessary. [0003] Considering the promotion and selection of vancomycin-resistant intestinal flora (especially enterococci), metronidazole is recommended as initial therapy. Metronidazole has significant side effects, including nausea, neuropathy, leukopenia, seizures, and toxic reactions to alcohol. Also, this medicine is not safe for use ...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/7048A61K47/38A61K47/32A61P31/04
Inventor 袁建栋
Owner BRIGHTGENE BIO MEDICAL TECH (SUZHOU) CO LTD
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